Intramolecular aminolysis of trichloroethyl esters: a mild macrocyclization protocol for the preparation of cryptophycin derivatives

被引：23

作者：

Fray, AH ^{[1
]}

机构：

[1] Lilly Res Labs, Chem Proc R&D, Indianapolis, IN 46285 USA

来源：

TETRAHEDRON-ASYMMETRY | 1998年 / 9卷 / 16期

关键词：

D O I：

10.1016/S0957-4166(98)00287-0

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

The bifunctional catalyst 2-hydroxypyridine (2-pyridone) is shown to promote the intramolecular aminolysis of the polyfunctionalized long-chain amino trichloroethyl ester 8 to afford cryptophycin-51 (4). This process for the construction of the macrocyclic core of cryptophycin derivatives is noteworthy for its convenience, avoidance of expensive coupling reagents, and use of mild reaction conditions. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：2777 / 2781

页数：5

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